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    Lipid lowering alkylene glycols and ester derivatives thereof
    4.
    发明授权
    Lipid lowering alkylene glycols and ester derivatives thereof 失效
    脂质降解亚烷基二醇及其酯衍生物

    公开(公告)号：US4275068A

    公开(公告)日：1981-06-23

    申请号：US48536

    申请日：1979-04-23

    申请人： Kurt Thiele ,  Quazi Ahmed ,  Ulrich Jahn ,  Rudolf Adrian

    发明人： Kurt Thiele ,  Quazi Ahmed ,  Ulrich Jahn ,  Rudolf Adrian

    IPC分类号： C07D213/80 ,  A61K31/455 ,  A61K31/60 ,  C07C69/90

    CPC分类号： C07D213/80

    摘要： Novel alkylene glycol derivatives of the formula (1) ##STR1## in which R.sup.1 is the hydrogen atom, an alkyl group having 1-4 C-atoms or an aryl group, R.sup.2 is the hydrogen atom or an alkyl group having 1-4 C-atoms, R.sup.3 is the hydrogen atom or a group of the formula ##STR2## in which Z is an alkyl residue, an optionally substituted aryl residue or a heterocyclic residue and R.sup.4 is a residue of the formula ##STR3## in which R.sup.5 is the hydrogen atom or chlorine atom, or the methyl group, exhibit an advantageous activity in regard of lowering the cholesterol and triglyceride level in the blood. Production of the novel derivatives by reduction of the corresponding acids, or by reacting a phenol of the formula ##STR4## and an alcohol of the formula ##STR5## optionally with subsequent esterification, is described.

    摘要翻译： 式（1）的新型亚烷基二醇衍生物其中R1是氢原子，具有1-4个碳原子的烷基或芳基，R2是氢原子或具有1个碳原子的烷基 -4个C原子，R3是氢原子或其中Z是烷基残基，任选取代的芳基残基或杂环残基的式“IMAGE”的基团，R4是式“IMAGE”的残基，其中 R5是氢原子或氯原子或甲基，在降低血液中的胆固醇和甘油三酯水平方面表现出有利的活性。 描述了通过还原相应的酸或通过使式（IMAGE）的酚与式（IMAGE）的醇任选地随后的酯化反应制备新衍生物。

    Phenoxy alkanoic acid derivatives having the ability to lower the level of fatty substances in the blood
    5.
    发明授权
    Phenoxy alkanoic acid derivatives having the ability to lower the level of fatty substances in the blood 失效
    具有降低血液中脂肪物质水平的能力的苯氧基链烷酸衍生物

    公开(公告)号：US4483999A

    公开(公告)日：1984-11-20

    申请号：US773148

    申请日：1977-03-01

    申请人： Kurt Thiele ,  Quazi Ahmed ,  Rudolf Adrian ,  Ulrich Jahn

    发明人： Kurt Thiele ,  Quazi Ahmed ,  Rudolf Adrian ,  Ulrich Jahn

    IPC分类号： C07C59/68 ,  C07C59/70 ,  C07C69/712 ,  C07D211/46 ,  C07D473/08 ,  C07C69/76

    CPC分类号： C07C321/00 ,  C07C59/68 ,  C07C59/70 ,  C07D211/46 ,  C07D473/08

    摘要： Novel compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, halogen, or alkyl or alkoxy containing from 1 to 4 carbon atoms,R.sup.2 is hydrogen, halogen, hydroxy or alkyl of alkoxy containing from 1 to 4 carbon atoms,n and m are integers such that the sum (n+m) lies in the range from 3 to 10 inclusive and n differs from m, andx is alkyl containing from 1 to 4 carbon atoms, hydrogen or a cation which is a metal cation of main Groups 1, 2 and 3 of the Periodic System of the Elements, an organic base cation or an ammonium ion. These compounds have pharmaceutical utility by virtue of their considerable ability to reduce the level of fatty substances in the blood.

    摘要翻译： 式中，R 1为氢，卤素，含有1至4个碳原子的烷基或烷氧基，R2为氢，卤素，羟基或含有1至4个碳原子的烷氧基烷基，n和m的新型化合物 整数，使得和（n + m）在3〜10的范围内，n与m不同，x是含有1〜4个碳原子的烷基，氢或作为主体1的金属阳离子的阳离子 ，元素周期系统的2和3，有机碱性离子或铵离子。 这些化合物由于其相当的降低血液中脂肪物质含量的能力而具有药用效用。

    Cholesterol-lowering phenoxyalkanoic acid esters
    6.
    发明授权
    Cholesterol-lowering phenoxyalkanoic acid esters 失效

    公开(公告)号：US4153803A

    公开(公告)日：1979-05-08

    申请号：US773144

    申请日：1977-03-01

    申请人： Kurt Thiele ,  Quazi Ahmed ,  Rudolf Adrian ,  Ulrich Jahn

    发明人： Kurt Thiele ,  Quazi Ahmed ,  Rudolf Adrian ,  Ulrich Jahn

    IPC分类号： A61K31/22 ,  C07C59/68 ,  C07C59/70 ,  C07C69/712 ,  C07C69/736 ,  C07D211/46 ,  C07D213/30 ,  C07D473/08 ,  C07C69/76

    CPC分类号： C07C321/00 ,  C07C59/68 ,  C07C59/70 ,  C07D211/46 ,  C07D473/08

    摘要： Compounds possessing pharmaceutical activity as substances able to lower the level of fatty substances in the blood possess the following general formula: ##STR1## wherein R represents hydrogen, halogen, hydroxy or alkyl or alkoxy containing from 1 to 4 carbon atoms;A.sup.1 and A.sup.2 which can be the same or different are hydrogen or alkyl containing from 1 to 9 carbon atoms such that A.sup.1 and A.sup.2 contain together not more than 10 carbon atoms,Y is oxygen, in which case X is benzyl, benzyloxy or benzylthio or benzyl, benzyloxy or benzylthio substituted by R and Z is amine, azacyclohydrocarbyloxy cycloalkoxy containing from 3 to 6 ring carbon atoms or tertiary aminoalkoxy or pivaloyloxyalkoxy in which the alkoxy group contains from 1 to 3 carbon atoms, or X is hydrogen and Z is pivaloyloxyalkoxy in which the alkoxy group contains from 1 to 3 carbon atoms, orY is oxygen, X is benzyl, benzyloxy or benzylthio or benzyl, benzyloxy or benzylthio substituted by R and Z is alkoxy containing from 1 to 4 carbon atoms, hydroxy or O.sup.- M.sup.+, M being a metal cation of Main Groups I, II or III of the Periodic System of the Elements or an organic base cation or ammonium ion, A.sup.1 and A.sup.2 being the same and being as aforesaid or being different with one of A.sup.1 and A.sup.2 being hydrogen or both being hydrogen and X being a para substituent with respect to Y in the benzene ring in the same general formula,Y is oxygen, X is hydrogen and Z is amine, azacyclohydrocarbyloxy or pivaloyloxyalkoxy in which the alkoxy group contains from 1 to 3 carbon atoms,Or Y is sulphur, in which case X is hydrogen, benzyl, benzyloxy or benzylthio or benzyl, benzyloxy or benzylthio substituted by R and Z is amine, azacyclohydrocarbyloxy, alkoxy containing from 1 to 4 carbon atoms, hydroxy, O.sup.- M.sup.+ wherein M is a metal cation of Main Groups I, II or III of the Periodic System of The Elements or an organic base cation or ammonium ion, cycloalkoxy containing from 3 to 6 ring carbon atoms or tertiaryaminoalkoxy, pivaloyloxyalkoxy or pyridyl-C-alkoxy in which the alkoxy group contains from 1 to 3 carbon atoms, and pharmacologically acceptable acid addition and quaternary ammonium salts of compounds containing basic groups, and optical isomers of said compounds when A.sup.1 and A.sup.2 are different.

    Theophylline derivatives
    7.
    发明授权
    Theophylline derivatives 失效
    茶碱衍生物

    公开(公告)号：US4603204A

    公开(公告)日：1986-07-29

    申请号：US474230

    申请日：1983-03-11

    申请人： Kurt Thiele ,  Felix Geissmann ,  Ludwig Zirngibl ,  Ulrich Jahn

    发明人： Kurt Thiele ,  Felix Geissmann ,  Ludwig Zirngibl ,  Ulrich Jahn

    IPC分类号： A61K31/52 ,  A61K31/522 ,  A61P25/02 ,  A61P29/00 ,  A61P37/08 ,  A61P43/00 ,  C07D295/22 ,  C07D307/02 ,  C07D473/08

    CPC分类号： C07D473/08

    摘要： New derivatives of theophylline having the formula ##STR1## in which R denotes hydrogen or OH, n the numbers 0 or 1, X either >CH-- or >N--, Y either --O-- or --CO-- and R a five membered or six membered aryl ring or hetero-aryl ring, that is substituted in given cases with halogen, short chain alkyl groups, alkoxy groups or halogen-alkyl, and exhibit in addition to other properties, histamine-, serotinine- bradykynine- antagonistic, anti-anaphylactic and -adrenergic stimulating effects.

    摘要翻译： 具有式（I）的茶碱的新衍生物，其中R表示氢或OH，n为数字0或1，X或> CH-或> N-，Y为-O-或-CO-，R a 在给定的情况下被卤素，短链烷基，烷氧基或卤素 - 烷基取代的五元或六元芳基环或杂芳基环，并且除了其它性质外，还表现出组胺，血清素 - 卡那霉素拮抗剂 ，抗过敏和肾上腺素能刺激作用。

    1H- and 2H- indazole derivatives
    8.
    发明授权
    1H- and 2H- indazole derivatives 失效
    1H-和2H-吲唑衍生物

    公开(公告)号：US4436913A

    公开(公告)日：1984-03-13

    申请号：US375116

    申请日：1982-04-28

    申请人： Istvan Molnar ,  Kurt Thiele ,  Felix Geissmann ,  Ulrich Jahn

    发明人： Istvan Molnar ,  Kurt Thiele ,  Felix Geissmann ,  Ulrich Jahn

    IPC分类号： C07D231/56 ,  C07D231/16 ,  C07D403/00 ,  C07D403/12

    CPC分类号： C07D403/12

    摘要： 1H- and 2H- indazole derivatives and pharmaceuticals containing these blood-pressure lowering 1H- and 2H- indazole derivatives of the formula ##STR1## and their acid addition salts, wherein R1 may be in position 1 or position 2 on the nitrogen atoms in formula I. The groups R1, R2 and R3 represent hydrogen or the usual lower molecular groups. The R group is a 2-imidazolinylamino group or a 3,4,5,6-tetryhydropyrimidinylamino group, wherein these groups may also be present in their tautomeric forms. These groups may also be in an aryl group in the R1 group, in which case the R group may also be a halogen atom. R may only represent one of the heterocyclic secondary or tertiary amino groups in the 4 or 7 position for the 1H- indazole derivatives when the R1 group is simultaneously an aryl or an aralkyl group.

    摘要翻译： PCT No.PCT / EP80 / 00094 Sec。 371日期1982年4月28日 102（e）日期1982年4月28日PCT提交1980年9月5日PCT公布。 出版物WO82 / 0082400 日期：1982年3月18日1 H-和2H-吲唑衍生物和含有这些降血压的1H-和2H-吲唑衍生物及其酸加成盐的药物，其中R1可位于1位 或位置2在式I中的氮原子上。基团R 1，R 2和R 3表示氢或通常的较低分子基团。 R基团是2-咪唑啉基氨基或3,4,5,6-四氢嘧啶基氨基，其中这些基团也可以它们的互变异构形式存在。 这些基团也可以是R 1基团中的芳基，在这种情况下，R基团也可以是卤素原子。 当R1基团同时为芳基或芳烷基时，R可以仅代表1H-吲唑衍生物的4或7位杂环仲或叔氨基之一。

    Antihypertensive 4-(2-imidazolin-2-yl-amino)-2-methyl-indazole
    9.
    发明授权
    Antihypertensive 4-(2-imidazolin-2-yl-amino)-2-methyl-indazole 失效
    抗高血压4-（2-咪唑啉-2-基 - 氨基）-2-甲基 - 吲唑

    公开(公告)号：US4526898A

    公开(公告)日：1985-07-02

    申请号：US530145

    申请日：1983-09-07

    申请人： Istvan Molnar ,  Kurt Thiele ,  Felix Geissmann ,  Ulrich Jahn

    发明人： Istvan Molnar ,  Kurt Thiele ,  Felix Geissmann ,  Ulrich Jahn

    IPC分类号： C07D403/12 ,  A61K31/415

    CPC分类号： C07D403/12

    摘要： 4-(2-Imidazolin-2-yl-amino)-2-methyl-indazole is a highly selective and effective .alpha..sub.2 -antagonist, .alpha..sub.1 -partial agonist and .alpha..sub.1s -agonist and displays anti-hypertensive activity and antagonistic activity on adrenaline and noradrenaline. It is useful as an .alpha.-adrenoceptor influencing and as an anti-hypertensively active drug.

    摘要翻译： 4-（2-咪唑啉-2-基 - 氨基）-2-甲基 - 吲唑是一种高选择性和有效的α2拮抗剂，α1-部分激动剂和α1s激动剂，并且对抗高血压活性和拮抗活性 肾上腺素和去甲肾上腺素。 作为α肾上腺素能受体影响作为抗高血压活性药物是有用的。

    Xanthine oxidase inhibitor and therapeutic treatment using same
    10.
    发明授权
    Xanthine oxidase inhibitor and therapeutic treatment using same 失效
    黄嘌呤氧化酶抑制剂及其治疗方法

    公开(公告)号：US4305942A

    公开(公告)日：1981-12-15

    申请号：US201500

    申请日：1980-10-28

    申请人： Kurt Thiele ,  James S. G. Cox ,  Johanna Fischer ,  Ulrich Jahn

    发明人： Kurt Thiele ,  James S. G. Cox ,  Johanna Fischer ,  Ulrich Jahn

    IPC分类号： A61K31/53 ,  A61K31/535 ,  A61P19/06 ,  A61P43/00 ,  C07D487/04

    CPC分类号： C07D487/04 ,  A61K31/00

    摘要： Therapeutic xanthine oxidase inhibitor composition containing as an active ingredient 3-dimethylamino-7-methyl-1,2-(n-propylmalonyl)-1,2-dihydro-1,2,4-benzotriazine dihydrate of the formula ##STR1## Uratic diathesis in warm-blooded animals is therapeutically treated by administering the aforementioned xanthine oxidase inhibitor to such animals, e.g., human, either orally or by means of an injection, thereby inhibiting their xanthine oxidase activity.

    摘要翻译： 含有下式的作为活性成分的3-二甲基氨基-7-甲基-1,2-（正丙基丙二酰基）-1,2-二氢-1,2,4-苯并三嗪二水合物的治疗性黄嘌呤氧化酶抑制剂组合物 通过以口服或注射方式向这些动物例如人类施用上述黄嘌呤氧化酶抑制剂来治疗温血动物的素质，由此抑制其黄嘌呤氧化酶活性。